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    Liposomes

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    neha
    Liposomes are concentric bilayer vesicles that can encapsulate aqueous volumes. They are formed from phospholipids that spontaneously assemble into closed structures when dispersed in water due to their amphiphilic properties. Liposomes can be classified based on lamellarity and size, and are characterized based on shape, size, surface charge, encapsulation efficiency, and phase behavior. They offer advantages for drug delivery such as selective targeting, increased efficacy and stability, and reduced toxicity.

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    Liposomes

    Uploaded by

    neha
    67 views42 pages
    Liposomes are concentric bilayer vesicles that can encapsulate aqueous volumes. They are formed from phospholipids that spontaneously assemble into closed structures when dispersed in water due to their amphiphilic properties. Liposomes can be classified based on lamellarity and size, and are characterized based on shape, size, surface charge, encapsulation efficiency, and phase behavior. They offer advantages for drug delivery such as selective targeting, increased efficacy and stability, and reduced toxicity.

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    liposomes formulation and evaluation

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    Liposomes are concentric bilayer vesicles that can encapsulate aqueous volumes. They are formed from phospholipids that spontaneously assemble into closed structures when dispersed in water due to their amphiphilic properties. Liposomes can be classified based on lamellarity and size, and are characterized based on shape, size, surface charge, encapsulation efficiency, and phase behavior. They offer advantages for drug delivery such as selective targeting, increased efficacy and stability, and reduced toxicity.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    67 views42 pages

    Liposomes

    Uploaded by

    neha
    Liposomes are concentric bilayer vesicles that can encapsulate aqueous volumes. They are formed from phospholipids that spontaneously assemble into closed structures when dispersed in water due to their amphiphilic properties. Liposomes can be classified based on lamellarity and size, and are characterized based on shape, size, surface charge, encapsulation efficiency, and phase behavior. They offer advantages for drug delivery such as selective targeting, increased efficacy and stability, and reduced toxicity.

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    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
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    At a glance
    Powered by AI
    The key takeaways are that liposomes are vesicles composed of lipid bilayers that can be used for targeted drug delivery. They were discovered in 1960 and provide advantages like increased efficacy, stability, and targeting while reducing toxicity.

    The different types of liposomes discussed are multilamellar vesicles (MLVs), large unilamellar vesicles (LUVs), small unilamellar vesicles (SUVs), and some based on sphingolipids and sterols.

    Some techniques used for loading drugs into liposomes include passive loading techniques like solvent injection methods, detergent depletion, and active loading techniques using ion gradients.

    Liposomes

    Unit I
    M.pharmacy I
    Neha Srivastava
    Introduction
    Slide Title

    • Liposomes are cocentric bilayerd vesicles in


    which aquoues volume is entirely enclosed
    by a membraneous lipid bilayer.
    • 1960 by Bangham et.al.
    • Targeting and delivery system
    • Natural and synthetic phospholipids
    • diameter ranges from 80nm to 100um
    Introduction
    Slide Title

    Advantages
    • Provides selective passive targeting
    • Increase efficacy and therapeutic index
    • Increase stability via encapsulation
    • Reduction in toxicity
    • Site avoidance effect
    • Improved pharmacokinetics
    • Flexibility with site specific legands
    General structure of liposome
    .

    Lipid bilayer
    Mechanism of liposome formation
    Slide Title

    Physiochemical features of phospholipids


    • Ampiphillic molecules (Polar head and non
    polar tail)
    • Tail 2 Fatty acid chain 10-24 C
    and 0-6 double bonds
    • Polar end bind to phosphoric acid
    • Supramolecular structure
    • In water, they spontaneously form closed
    structures
    Mechanism of liposome formation
    Slide Title

    Physiochemical features of phospholipids


    • Self assembling of structure in aq medium
    • Amphiphilic molecules such as soap, detergents
    can also be used
    • In water they form different microscopic
    structures such as lamellar, hexagonal etc
    • Commonly used is natural phospholipid-
    phosphatidylcholine (PC)
    .

    Structure of
    the
    phospholipid
    molecule
    Mechanism of liposome formation
    Slide Title
    Phosphatidylcholine

    Glycerol group attached polar head and non polar tail


    Molecule of PC are not soluble but organize in aq environment
    Large free energy shift in aquoeus and hydrophobic environment
    State of lowest energy indicates highest stability
    Mechanism of liposome formation
    Slide Title

    Phosphitidylcholine
    • Soaps forms spherical micellar structure
    • Effect of phase transition temperature
    • Hydration of lipid bilayer
    • On agitation forms MLV
    • Sonication -small unilamilar vesicles
    • Mechanical energy – Large unilamilar vesicles
    2. SPHINGOLIPIDS

    • They contain sphingosine (or) a related base as


    their structural backbone.

    • They contain 3 characteristic building blocks:-


    - A molecule of fatty acid
    - A molecule of sphingosine &
    - Head groups that can vary from simple alcohol
    as choline to very complex carbohydrates.

    • The most abundant sphingolipid in higher animals


    is sphingomyelin.
    3. GLYCOSPHINGOLIPIDS
    • These are found mainly in grey matter of brain tissue
    of higher animals and are used in minor component.
    • These are included in liposomes formulation to
    provide a layer of surface charged groups.

    4. STEROLS
    • Cholesterol & its derivatives are quite often
    included as components of liposomal membrane.
    5. SYNTHETIC PHOSPHOLIPIDS
    • Saturated phospholipids include dipalmitoyl
    phosphatidyl choline(DPPC) , dipalmitoyl
    phosphatidyl ethanol amine(DPPE) , dipalmitoyl
    phosphatidyl serine(DPPS) .

    • Unsaturated phospholipids have also been used which


    include dioleo-phosphatidyl choline(DOPC) , dioleo-
    phosphatidyl glycerol(DOPG)
    6. POLYMERIC MATERIALS

    • A large variety of polymerizable lipids which can


    form vesicles , has been synthesized.

    • These include lipids containing conjugated diene ,


    methacrylate , and thiol groups as polymerizable
    moieties.
    Mechanism of liposome formation
    Slide Title
    • Effect of molecular geometry
    Mechanism of liposome formation
    Slide Title
    Rigidization of structure
    • Cholesterol modulate the bilayer membrane
    • Fluidity buffer
    • Above phase transition temperature it tends
    to make the membrane more order
    • Do not form bilayer but can trap in between
    • Orientation of cholesterol
    • Effect of Phage transition temperature
    • 1:1 is efficient
    Mechanism of liposome formation
    Slide Title
    Rigidization of structure
    • Cholesterol modulate the bilayer membrane
    • Fluidity buffer
    • Above phase transition temperature it tends
    to make the membrane more order
    • Do not form bilayer but can trap in between
    • Orientation of cholesterol
    • Effect of Phage transition temperature
    • 1:1 is efficient
    Classification of liposomes
    Slide Title
    Rigidization of structure
    • Cholesterol modulate the bilayer membrane
    • Fluidity buffer
    • Above phase transition temperature it tends
    to make the membrane more order
    • Do not form bilayer but can trap in between
    • Orientation of cholesterol
    • Effect of Phage transition temperature
    • 1:1 is efficient
    Slide Title
    Passive loading Techniques
    Mechanical dispersion method of passive
    loading
    • Lipid solution in organic phase
    • Removal of organic phase
    • Dry layer formation
    • Hydration
    • Different parameters such as vortexing,
    sonication, etc
    Slide Title
    Passive loading Techniques

    Thin film hydration by hand shaking(MLV)


    or Non shaking method (ULV)
    Slide Title
    Passive loading Techniques

    Proliposomes (MLV)
    Lipid is dried over the support
    Lipid + Support Dry film

    Proliposomes Hydration
    Slide Title
    Passive loading Techniques

    Mechanical treatment of MLVS


    Sonication (SUVs)
    • Reduce to SUVs
    • Two types : Bath and probe
    • Probe tip – high energy – liposomal degradation
    • Contribute titanium particles
    • Sonication for 5-10 min
    • Lipid dispersion clarifies
    Slide Title
    Passive loading Techniques

    Mechanical treatment of MLVS


    Sonication (SUVs)
    • Reduce to SUVs
    • Two types : Bath and probe
    • Probe tip – high energy – liposomal degradation
    • Contribute titanium particles
    • Sonication for 5-10 min
    • Lipid dispersion clarifies – further Centrifugation
    Slide Title
    Passive loading Techniques

    Mechanical treatment of MLVS


    Sonication (SUVs)
    • Reduce to SUVs
    • Two types : Bath and probe
    • Probe tip – high energy – liposomal degradation
    • Contribute titanium particles
    • Sonication for 5-10 min
    • Lipid dispersion clarifies – further Centrifugation
    Slide Title
    Passive loading Techniques
    Slide Title
    Passive loading Techniques

    French pressure cell liposome


    • Reduce to SUVs
    • Two types : Bath and probe
    • Probe tip – high energy – liposomal degradation

    • Contribute titanium particles


    • Sonication for 5-10 min
    • Lipid dispersion clarifies – further Centrifugation
    Passive
    Slide loading Techniques
    Title

    French pressure cell liposome


    • Uni or oligo lamellar liposomes
    • More stable
    • Lipid phase composition, temperature and
    pressure
    • Low leakage
    • Less heterogenicity
    Passive
    Slide loading Techniques
    Title

    Micro Emulsion Liposome


    • Microfludizer SUV
    Passive
    Slide loading Techniques
    Title

    Vesicle produced by extrusion techniques


    • LUV and MLV
    Passive
    Slide loading Techniques
    Title

    Dried reconstituted vesicles


    Freeze thaw cycle
    Passive
    Slide loading Techniques
    Title

    Liposomes from pre formed vesicles


     pH induced
     Calcium induced
     Cochleate method
    Passive
    Slide loading Techniques
    Title

    SOLVENT DISPERSION METHOD


    Ethanol Injection
    Passive
    Slide loading Techniques
    Title

    SOLVENT DISPERSION METHOD


    Ether Injection
    Passive
    Slide loading Techniques
    Title

    SOLVENT DISPERSION METHOD


    Ether Injection
    Passive
    Slide loading Techniques
    Title

    Rapid solvent exchange vesicles


    Organic solution of lipid is added with syringe
    to aq phase under vacuum
    Passive
    Slide loading Techniques
    Title

    De-emulsification method
    Double emulsion vesicles
    Reverse phase evaporation vesicles
    Passive
    Slide loading Techniques
    Title

    DETERGENT DEPLETION
    • Micelles formation
    • Dialysis
    • Column chromatography
    • Detergent adsorption using bio beads
    ActiveTitle
    Slide loading Techniques

    DETERGENT DEPLETION
    • Ion transport
    • Weak acid or base
    • High encapsulation
    • Reduced leaking
    • Bed side laoding of drug
    ActiveTitle
    Slide loading Techniques

    • Ion transport
    • Weak acid or base
    • High encapsulation
    • Reduced leaking
    • Bed side laoding of drug
    Removal
    Slide Titleof untrapped drugs

    • MLVs compared to LUVs and SUVs


    • Centrifugation
    • Supernatant contains untrapped drugs
    Characterization
    Slide Title of liposomes

    Vesicle shape and Lamellarity


    • Electron microscope technique

    Lamellarity
    • Freeze facture electron microscopy
    • 31 P nuclear magnetic resonance
    Characterization
    Slide Title of liposomes

     Vesicle size and distribution


     Light microscopy
     Fluorescent Microscopy
     Electron microscopy
     TEM
     Lazer light scattering
     Zetasizer
    Characterization
    Slide Title of liposomes

    Surface charge
    Encapsulation efficiency
    Trapped volume
    Phase behaviour

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